Docetaxel (docetaxel, DTX) is a taxol antineoplastic drug with a molecular formula of C43H53NO14 and a molecular weight of 807.88, which may be combined with a free tubulin to promote the tubulin to be assembled into a stable microtubule, and meanwhile suppress the depolymerization of the tubulin, and cause the generation of a microtubule bundle losing normal functions and fixation of the microtubule, thus suppressing cell mitosis and playing an antineoplastic role. Docetaxel is clinically applied to breast cancer, non-small cell lung cancer, pancreatic cancer, soft tissue sarcoma, head and neck cancer, stomach cancer, ovarian cancer and prostatic cancer or the like, and has notable curative effects no matter it is applied alone or in combination.
However, the docetaxel has such defects like poor water solubility, short half life period and high toxicity at the same time, which limit its clinic applications. At present, docetaxel injections commercially available at home and abroad are prepared by dissolving docetaxel in Tween-80, and need to be diluted using a specialized solvent for injection strictly during clinic application. Its operation requirements are strict and its use method is tedious. Moreover, a large amount of Tween contained in the preparation is easy to cause such adverse reactions as hemolysis and allergy or the like, which needs to take such drugs like dexamethasone in advance for control, is inconvenient for clinic medication, and has low medication safety. So far, this problem has not been preferably solved yet.
A nano-polymer micelle is a drug carrier system developed in recent years direct to indissolvable drugs, which has a core-shell structure, wherein the core is a hydrophobic part, and the shell is a hydrophilic part. The polymer micelle may encapsulate the indissolvable drugs into the core part to solubilize the indissolvable drugs. Compared with a normal solubilizer and latent solvent, the polymer micelle drug carrier system has higher security since it selects biodegradable material as raw materials. Therefore, it has a better application prospect while being served as an encapsulating-carrying accessory for the indissolvable drugs. In multiple technologies, a micelle prepared by the methoxypolyethylene glycol-polylactic acid block copolymer block polymer and the docetaxel is applied to try to solve the difficulty; for example, CN201110105540 discloses a micelle prepared by a methoxypolyethylene glycol-polylactic acid block copolymer and docetaxel, which solves the solubilization problem of docetaxel.
However, the present micelle prepared by the methoxypolyethylene glycol-polylactic acid block copolymer and the docetaxel has poorer stability after being dispersed by water, and the drugs are leaked in a very short time, so that it cannot be further popularized and truly applied during clinic application since its physical stability is not high. In order to solve the problem, CN201010114289 discloses a technology which improves the stability of a micelle after re-dissolving through a method of adding amino acid in a polymer micelle, but the added substances have higher requirements on industrialized production, and a stabilizer added increases the technical complexity of the preparation, and meanwhile, the added amino acid plays a role of degrading the main drugs, which is not suitable for large-scale production.